摘要/Abstract

为了研究二萘并呋喃衍生物的构效关系，设计合成了两个系列的二萘[2，1-b：1'，2'-d]呋喃衍生物，通过¹H NMR、¹³C NMR、HRMS和IR数据对所有目标化合物进行了结构鉴定.通过噻唑蓝（MTT）法测试了目标化合物的体外抗肿瘤活性，大多数化合物对人肝癌细胞（HepG2和SMMC-7721）、人宫颈癌细胞（HeLa细胞）和急性早幼粒细胞白血病细胞（NB4细胞）显示了较强的抗肿瘤活性.其中N³，N¹¹-二羟基二萘并[2，1-b：1'，2'-d]呋喃-3，11-二甲酰胺（13k）对SMMC-7721细胞显示了很强抑制作用，其半数抑制浓度为0.57 μmol·L^－1，远低于阳性对照药5-氟脲嘧定的20.21 μmol·L^－1.
关键词: 合成设计, 细胞毒, 二萘并呋喃, 核磁光谱
In order to study the structure-activity relationships of dinaphthofuran derivatives, two series of dinaphtho[2,1-b:1', 2'-d]furan derivatives were synthesized. The structures of all compounds were identified by ¹H NMR, ¹³C NMR, HRMS and IR spectra. The in vitro antitumor activity of the synthesized derivatives was tested by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. Most of them exhibited strong inhibitory activity on human hepatocellular carcinoma cell lines (HepG2 and SMMC-7721 cells), uterine cervix cancer Hela cells and acute promyelocytic leukemia NB4 cells. Compound 13k exhibited significant inhibitory activity against SMMC-7721 cells with IC₅₀ vaue of 0.57 μmol·L^-1, much lower than 20.21 μmol·L^-1 of the positive control 5-Fu.
Key words: synthesis design, cytotoxicity, dinaphthofuran, NMR spectroscopy


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